Abstract: The present disclosure provides compounds of Formula (I) and Formula (II). The compounds described herein may be useful in treating proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.

Abstract: Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.

Abstract: The present description relates to methods of treating spinocerebellar ataxia type 3 (SCA3) using substituted thieno[3,2-d]pyrimidine compounds, forms, and pharmaceutical compositions thereof.

Abstract: The invention relates to compounds and methods of treating diseases including but not limited to, cancer, non-cancer proliferative disease, sepsis, autoimmune disease, viral infection, atherosclerosis, Type 1 or 2 diabetes, obesity, inflammatory disease, or Myc-dependent disorder including by modulating biological processes by the inhibition of cell cycle checkpoint targets CDKs, and/or PI3 kinase, and/or bromodomain protein binding to substrates, comprising the administration of a compound(s) of Formula 1-V1 (or pharmaceutically acceptable salts thereof) as defined herein.

Abstract: The present invention relates to new anthelmintic compounds. These compounds can for example be used in the treatment of the kind of worm disease caused by helminths such as Dirofilaria, in particular Dirofilaria immitis.

Abstract: Hydromorphone hydrochloride (I·HCl) is converted into hydromorphone base (I) via hydromorphone monohydrate (I·H2O).

Abstract: The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein W1, W2, Y, Z, M, L, Cy, Cz, R1, R2, R3, R4, R2a, Ry, Rz, and the subscripts m, n, q, and r are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

Abstract: A refining method of a midbody of latamoxef sodium includes: dissolving 7?-amino-7?-methoxy-3-(5-tetrazolyl)thiomethyl-1-oxa-3-cephem-4-carboxylic acid in dichloromethane, and then dividing into a dichloromethane layer and a water layer; extracting the dichloromethane layer, adding a NaHCO3 solution to stir, and remaining an organic layer after stratification; stirring, crystallizing and filtering the organic layer in turn, to obtain a filtrate, preparing a second powder by stirring the filtrate under conditions of a catalyst and a normal temperature; preparing a first powder by extracting the water layer, dropping the hydrochloric acid to adjust a pH value thereof, performing crystal cultivation and suction filtration after performing cooling, and then performing vacuum drying; combining the first powder and the second powder to prepare the midbody of latamoxef sodium: 7?3-amino-7?-methoxy-3-(5-tetrazolyl)thiomethyl-1-oxa-3-cephem-4-carboxylic acid, which has a yield of 95.6-96.8% and a purity of 99.2-99.5%.

Abstract: The invention relates to novel compounds for use as inhibitors of NLRP3 inflammasome production, wherein such compounds are as defined by compounds of formula (I) and wherein the integers R1, R2 and R3 are defined in the description, and where the compounds may be useful as medicaments, for instance for use in the treatment of a disease or disorder that is associated with NLRP3 inflammasome activity.

Abstract: The present invention provides compounds of the formula: wherein A, B, D1, X, Y, Z, G, R1, R2, and R3a are as described herein, pharmaceutically acceptable salts thereof, and methods of using these compounds and pharmaceutically acceptable salts thereof for treating patients for cancer.

Abstract: The present invention relates to a method of synthesizing copper (I) 5-nitrotetrazolate. The method involves a series of interconnected steps. Initially, a stock solution of sodium 5-nitrotetrazolate is prepared in water from 5-aminotetrazole nitrate, which is then preserved for later use in producing copper (I) 5-nitrotetrazolate thereby eliminating the need for immediate utilization. A nascent Copper (I) chloride is prepared separately. In a single step, the stock solution of sodium 5-nitrotetrazolate is coupled with the nascent copper (I) chloride, resulting in the formation of copper (I) 5-nitrotetrazolate.

Abstract: Specific heterocyclic compounds, a material, preferably an emitter material, for an organic electroluminescence device containing the specific heterocyclic compounds, an electronic equipment containing the organic electroluminescence device, a light emitting layer containing at least one host and at least one dopant, where the dopant contains at least one of the heterocyclic compounds, and the use of the heterocyclic compounds in an organic electroluminescence device.

Abstract: Embodiments of the present invention provide a method, comprising obtaining a lecithin-containing material, in some aspects derived from a crude refining stream, comprising 20-80 wt % acetone insoluble matter, 1-30 wt % free fatty acid, and less than 10 wt % water, adding a fatty acid or carboxylic source to the lecithin-containing material to obtain a lecithin fatty acid blend or lecithin carboxylic acid blend and incorporating the blend into asphalt or oil field applications.

Abstract: Compounds useful as fluorescent or colored dyes are disclosed. The compounds have the following structure (I): or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, R4, R5, L1, L3, L4, L6, L7, L8, M1, M2, q, w and n are as defined herein. Methods associated with preparation and use of such compounds are also provided.

Abstract: Provided are the crystalline solid meglumine salts of (R)-5-(4-chlorophenyl)-1-isopropyl-2-methyl-4-(3-(4-(4-((4-((1-(phenylthio)-4-(4-((phosphonooxy)methyl)piperidin-1-yl)butan-2-yl)amino)-3- ((trifluoromethyl)sulfonyl)phenyl)sulfonamido)phenyl) piperazin-1-yl)phenyl)-1H-pyrrole-3-carboxylic acid. Pharmaceutical compositions having one or more of the crystalline solid meglumine salt compounds and methods for administering the crystalline solid meglumine salt compounds to a subject are also described. Methods for preparing the crystalline solid meglumine salt compounds are also provided.

Abstract: Novel crystalline forms of brigatinib, pharmaceutical compositions comprising the same, and methods of their preparation and use of the same are disclosed herein.

Abstract: The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.

Abstract: Disclosed herein are methods of crystallizing the compound of Formula I, as well as crystalline forms thereof. Crystalline forms of Formula I disclosed include the TBME solvate crystalline form, toluene solvate crystalline form, ethanol solvate crystalline form, THF solvate crystalline form, EtOAc solvate crystalline form, acetone solvate crystalline form and crystalline Form C.

Abstract: The invention relates to novel platinum(II) complexes with C{circumflex over (?)}C* and borate ligands of the following formula (I), processes for their preparation and their use in OLEDs.

Abstract: A compound having a structure of Formula I, is provided. In Formula I, M is Pt or Pd; rings A, B, C, and D are 5-membered or 6-membered rings; one of Z1, Z2, and Z3 is N and the other two are C; each of X1 to X10 is C or N; K is a direct bond, O, S, N(R?), P(R?), B(R?), C(R?)(R?), or Si(R?)(R?); each of L1 and L2 is a direct bond or a linker; each R, R?, R?, R?, R?, RA, RB, RC, RD, and RE is hydrogen or a General Substituent; R1 is a substituent; at least one RE comprises a substituent selected from the group consisting of aryl, heteroaryl, cycloalkyl, and heteroalkyl; any two substituents may be joined or fused to form a ring, except that RE at X3 or X4 cannot be joined with RA to from a ring. Formulations, OLEDs, and consumer products including the compound are also provided.

Abstract: A light-emitting device includes: a first electrode; a second electrode facing the first electrode; an interlayer between the first electrode and the second electrode; and an organometallic compound of Formula 1: wherein Formula 1 is the same as described in the specification. The organometallic compound satisfies at least one of Conditions 1 or 2: Condition 1 the organometallic compound has a dipole moment of 3 Debye or less; and Condition 2 the organometallic compound has a horizontal orientation ratio of 90% or more.

Abstract: A continuous reaction system for preparing a ferromanganese oxalate precursor may comprise a first dissolution reactor, a second dissolution reactor, a first reactor, a second reactor, a material storage tank, and an ultrasonic reactor; the first dissolution reactor may be configured to accommodate a metal salt solution required for preparing the ferromanganese oxalate precursor, and the second dissolution reactor may be configured to accommodate a precipitant solution required for preparing the ferromanganese oxalate precursor; the first reactor may include a first feed port and a first overflow port, and the first feed port of the first reactor may be interconnected to a first discharge port of the first dissolution reactor and a second discharge port of the second dissolution reactor respectively through two pipelines.

Abstract: Provided herein are methods and catalysts for the production of hexoses, pentoses, tetroses, trioses, ketoses, heptoses, aldehydes, glycolaldehyde, and glyceraldehyde from carbon dioxide using a system that does not rely on biological production methods. The process first converts carbon dioxide into an aldehyde intermediate, which is secondly used as feedstock to produce larger aldehydes and sugars in a formose reaction. The resulting process is a useful CO2 utilization method for space exploration and in-situ resource utilization, with potential application for terrestrial production of low-carbon chemicals.

Abstract: Disclosed are co-crystal forms of N-(2-(5-(((2R,3R,4S,5R)-3,4-dihydroxy-5-methoxy-6,6-dimethyltetra-hydro-2H-pyran-2-yl)oxy)-3?-fluoro-[1,1?-biphenyl]-2-yl)ethyl)-acetamide and L-proline or D-proline, their pharmaceutical compositions, processes of manufacture, and methods of use for treating neurodegenerative disorders such as diabetic peripheral neuropathy.

Abstract: The present disclosure relates to solid forms (e.g. crystalline forms, solvates, and crystalline forms thereof) of a compound which is ((2R,3S,4R,5R)-5-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2-yl)methyl neopentyl carbonate, which is useful in the treatment of treating viral infections, for example paramyxoviridae, pneumoviridae, picornaviridae, flaviviridae, filoviridae, arenaviridae, orthomyxovirus, and coronaviridae infections.

Abstract: Disclosed are 5?-substituted nucleoside monophosphates, which contain 5-fluorouracil or 5-fluorothiouracil as the nucleobase. In general, the 5?-substituted nucleoside monophosphates disclosed herein can inhibit human thymidylate synthase and thereby possess anti-cancer therapeutic effects. The 5?-substitution in these nucleoside monophosphates can prevent metabolic cleavage of the monophosphate group, mediated by enzymes such as 5?-nucleotidases, phospholipase D, etc. This feature can improve metabolic profiles, enhance target specificity, and/or reduce side effects of these compounds, compared to their corresponding unsubstituted analogs. Also disclosed are prodrugs of these 5?-substituted nucleoside monophosphates. After administration, the prodrugs can be metabolized to release their corresponding 5?-substituted nucleoside monophosphates. Methods of treating cancer using the 5?-substituted nucleoside monophosphates and prodrugs thereof are disclosed.

Abstract: There is disclosed a composition comprising a first construct, wherein the first construct comprises a charge component, a lock component and a key component; wherein the lock component and the key component are specific affinity binding partners and are separated such that they are unable to form a binding pair within the same construct; whereby in a first environmental condition, the charge component imparts a first overall charge to the first construct, the lock component binds to its binding partner on a second construct, and the key component binds to its binding partner on a third construct; and whereby in a second environmental condition, the charge component imparts a second overall charge to the first construct, and the lock and key components are in an unbound state. Also disclosed is a method of purification of a target compound involving the composition.

Abstract: The present invention relates to the surprising discovery that previous hemoglobin-based drug purification methodologies do not remove sufficient endotoxins exposures at the various steps which may complex with the hemoglobin protein. These complexed endotoxins can result in serious health complications (e.g. development of cardiac lesions for one). Additionally, varied endotoxin types and concentration contributes to batch-to-batch variability during hemoglobin-based drug manufacture. Endotoxins are not as much of an issue for peptides as compared to larger protein complexes. Accordingly, the instant disclosure is directed to a purification process using single use systems in many process steps including high performance chromatography systems thereby removing endotoxins while keeping processing costs low.

Abstract: The compounds of the present invention are represented by the following compounds having Formula I and Formula (I?): where the substituents R1, R2, R2?, R3, R4, R5, R?, R?, X, Y, and Z are as defined herein and where the substituents R1, R2, R3, R4, R5, R?, R?, X, Y, and Z are as defined herein. These compounds are used in the treatment of bacterial infections, parasite infections, fungal infections, cancer, immunologic disorders, autoimmune disorders, neurodegenerative diseases and disorders, inflammatory disorders, or muscular dystrophy or for providing immunosuppression for transplanted organs or tissues.

Abstract: There is provided a method of synthesizing the tetrapeptide exhibiting an anti-wrinkle activity consisting of the amino acid sequence of glycine(Gly)-glutamine(Gln)-valine(Val)-serine(Ser) (SEQ ID NO: 1). The method includes: preparing a peptidyl resin by utilizing 2-(4-nitrophenyl) sulfonylethoxycarbonyl-amino acid (Nsc-amino acid); adding an eluting solution to the prepared resin; and filtering the resin and obtaining the tetrapeptide.

Abstract: The present disclosure relates to synthesis and characterization of novel polymorphic forms of Cyclo (-His-Pro) (“CHP”).

Abstract: Provided are compositions and methods for treating progressive neurological childhood symptoms and conditions associated with lysosomal storage disorders (LSD) such as neurological mucopolysaccharidoses. The compositions may include nootropic peptides such as Semax, which can be N-terminally acetylated and/or C-terminally amidated. The peptides can be effectively delivered by intranasal administration into the brain parenchyma, where they exert a neuroprotective and anti-inflammatory effect and delay or restore neuropathophysiological defects such as neuropsychiatric problems, developmental delays, mental retardation and dementia.

Abstract: The present invention relates to an anti-inflammatory peptide for preventing or treating atopic dermatitis, and specifically, the present invention provides: a peptide or fragment thereof consisting of an amino acid sequence selected from the group consisting of SEQ ID NO: 1 to SEQ ID NO: 17, or a conjugate thereof; and a pharmaceutical composition and a cosmetic composition for preventing or treating atopic dermatitis comprising the peptide or fragment thereof, etc. as an active ingredient. The peptide or fragment thereof, or a conjugate thereof, has excellent anti-inflammatory activity, and thus is safe from the side effects of existing therapeutic agents for atopic dermatitis, and can effectively prevent, ameliorate, or treat atopic dermatitis.

Abstract: Methods and compositions related to the selective, specific disruption of multiple ligand-receptor signaling interactions, such as ligand-receptor interactions implicated in disease, are disclosed. These interactions may involve multiple cytokines in a single receptor family or multiple ligand receptor interactions from at least two distinct ligand-receptor families. The compositions may comprise polypeptides having composite sequences that comprise sequence fragments of two or more ligand binding sites. The methods and compositions may involve sequence fragments of two or more ligand binding sites that are arranged to conserve the secondary structure of each of the ligands from which the sequence fragments were taken.

Abstract: The present invention provides a peptide that consists of an amino acid sequence with 20 or fewer residues containing at least one amino acid sequence selected from the group consisting of the amino acid sequence represented in SEQ ID NO: 1, the amino acid sequence represented in SEQ ID NO: 2 and the amino acid sequence represented in SEQ ID NO: 38, the peptide having an activity to inhibit proliferation of a tumor cell or having an activity to inhibit binding between an epidermal growth factor receptor and a signal-transducing adaptor family member-2 (STAP-2); a peptide with a cell-penetrating peptide added to a terminus of the above peptide with or without a linker sequence interposed between the cell-penetrating peptide and the terminus; and pharmaceutical compositions containing any of these peptides.

Abstract: The disclosure related to therapeutic proteins and pharmaceutical compositions comprising said proteins, which have utility in treating various human diseases. In particular aspects, the disclosed therapeutic proteins are useful for treating human gastrointestinal inflammatory diseases and gastrointestinal conditions associated with decreased epithelial cell barrier function or integrity. Further, the disclosed therapeutic proteins are useful for treating human inflammatory bowel disease, including inter alia, Crohn's disease and ulcerative colitis.

Abstract: An object of the present invention is to provide a polypeptide having excellent alkaline stability and also allowing an immunoglobulin or a fragment thereof that has been bound to be eluted in a weakly acidic range, by modifying an amino acid sequence of an immunoglobulin-binding domain of Protein A. By substitution of serine at position 41 with an amino acid with a hydrophobic side chain, tyrosine, or histidine in each immunoglobulin-binding domain of Protein A, a polypeptide is obtained having avidity for an immunoglobulin or a polypeptide containing an Fc region thereof, having excellent alkaline stability, and also allowing the immunoglobulin or the polypeptide containing an Fc region thereof that has been bound to be efficiently eluted under weakly acidic mild conditions.

Abstract: Compositions including an antibiotic factor from Malassezia are provided. In some examples, the compositions include a Malassezia exoproduct, a Malassezia cell-free supernatant, or a Malassezia cell and a pharmaceutically acceptable carrier. Methods of treating an infection in a subject, such as a Staphylococcus infection are also provided.

Abstract: Provided herein are compositions and methods for the treatment of cancer by activating the spindle assembly checkpoint (SAC) in cells. In particular, dimerized Mps1 and Spc105/KNL1 constructs are provided as tunable activators of SAC, allowing for control of chromosome segregation accuracy and prevention of aneuploidies that are common in cancer.

Abstract: Described herein are proteins comprising an ankyrin repeat domain with a mutation in the N-terminal capping module, in particular a mutation at position 24 of the N-terminal capping module, as well as related products and methods.

Abstract: The invention provides inhibitors of interferon regulatory factor 5 FIG. 5 (IRF5) nuclear localization and methods of using the inhibitors to treat autoimmune diseases such as systemic lupus erythematosus (SLE).

Abstract: The present disclosure provides biosensor cells and methods of use thereof. The disclosure provides, for example, methods of measuring a titer of or of detecting a seed tau protein in a sample, methods of detecting Alzheimer's disease (AD), or a neurodegenerative tauopathy disease or condition linked to tau protein aggregation, and methods for the identification of putative tau protein aggregation inhibitors or modulators.

Abstract: Described herein are polypeptides comprising an FGF17, IGF2, or BMP7 amino acid sequence and an amino acid sequence from a heterologous polypeptide useful for the treatment of soft-tissue and muscle diseases, disorders, and injuries. Also described herein are synergistic combinations of a Fibroblast Growth Factor Receptor agonist and a glycosaminoglycan, an Insulin-like Growth Factor 1 Receptor (IGF1R) agonist and a short chain fatty acid, and BMP receptor agonists and mTOR activators and/or glycosaminoglycans. Also described are methods of treating muscle and soft-tissue diseases comprising administering the polypeptides and/or synergistic compositions.

Abstract: The invention relates to a polypeptide selected from bone morphogenetic protein 10 (BMP10), or a bone morphogenetic protein 9 (BMP9) variant lacking osteogenic activity, for use in the treatment of a vascular disease or a respiratory disease. The invention also relates to novel BMP9 variants and to pharmaceutical compositions comprising said polypeptides.

Abstract: The present disclosure relates to a manufacturing process of sargramostim, which results in improved yield efficiency and output.

Abstract: The present invention relates to a novel interleukin-21 (IL-21) mutant protein and use thereof. In particular, the present invention relates to an IL-21 mutant protein that has improved properties, such as a reduced binding property to an IL-21 receptor and improved druggability, compared to wild-type IL-21. The present invention also provides a fusion comprising the IL-21 mutant protein, a nucleic acid encoding the IL-21 mutant protein or the fusion, and a vector and a host cell comprising the nucleic acid. The present invention further provides a method for preparing the IL-21 mutant protein or the fusion, a pharmaceutical composition comprising the same, and therapeutic use.

Abstract: Provided herein are IL-12 polypeptide complexes and/or IL23 polypeptide complexes comprising IL-12 or IL-23, a half-life extension element, an IL-12 or IL-23 blocking element and a protease cleavable linker. Also provided herein are pharmaceutical compositions thereof, as well as nucleic acids, recombinant expression vectors, host cells for making such polypeptide complexes. Also disclosed are methods of using the polypeptide complexes in the treatment of diseases, conditions and disorders.

Abstract: This disclosure relates to protease-cleavable cytokine prodrugs. In some embodiments, the prodrugs comprise a targeting sequence. In some embodiments, the prodrugs comprise a pharmacokinetic modulator.

Abstract: Provided herein are targeted cytokine constructs and method of engineered cell therapy by administering a targeted cytokine construct in combination with an engineered cell therapy, for use in treating a disease, e.g., a proliferative disease, e.g., a cancer.

Abstract: Provided herein are IL-2 muteins that bind to IL-2 receptor subunit but do not have measurable binding to IL-2 receptor subunit. Also provided are compositions, kits, methods, and uses involving such IL-2 muteins.